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    • 1. 发明授权
      US06187786B1 Farnesyl transferase inhibiting 1,8-annelated quinolinone derivatives substituted with N- or C-linked imidazoles 有权
    • Farnesyl transferase inhibiting 1,8-annelated quinolinone derivatives substituted with N- or C-linked imidazoles
    • 抑制由N-或C-连接的咪唑取代的1,8-环化喹啉酮衍生物的法呢基转移酶
    • US06187786B1
    • 2001-02-13
    • US09380856
    • 1999-12-20
    • Marc Gaston Venet , Patrick René Angibaud , Yannick Aimé Eddy Ligny , Virginie Sophie Poncelet , Gerard Charles Sanz
    • Marc Gaston Venet , Patrick René Angibaud , Yannick Aimé Eddy Ligny , Virginie Sophie Poncelet , Gerard Charles Sanz
    • A61K31473
    • C07D471/06 , C07D455/04
    • This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; —A— is a bivalent radical of formula; R1 and R2 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar, Ar—C1-6alkyl, Ar-oxy, Ar—C1-6alkyloxy; or when on adjacent positions R1 and R2 taken together may form a bivalent radical; R3 and R4 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy, Ar-oxy, C1-6alkylthio, di(C1-6alkyl)amino, trihalomethyl, trihalomethoxy, or when on adjacent positions R3 and R4 taken together may form a bivalent radical; R5 is an imidazolyl substituted with hydrogen or C1-6alkyl; R6 hydrogen, hydroxy, halo, cyano, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl or Ar; or a radical of formula —O—R7, —S—R8, —N—R8R9; and Ar is optionally substituted phenyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
    • 本发明涉及配制药学上可接受的酸加成盐和其立体化学异构形式的化合物，其中虚线表示任选的键; X是氧或硫; -A-是式的二价基团; R 1和R 2各自独立地为氢，羟基，卤素，氰基，C 1-6烷基，三卤代甲基，三卤甲氧基，C 2-6烯基，C 1-6烷氧基，羟基C 1-6烷氧基，C 1-6烷氧基C 1-6烷氧基，C 1-6烷氧基羰基，氨基C 1-6烷氧基， 或二（C 1-6烷基）氨基C 1-6烷氧基，Ar，Ar-C 1-6烷基，Ar-氧基，Ar-C 1-6烷氧基; 或者当在相邻位置R1和R2一起可以形成二价基团时; R 3和R 4各自独立地为氢，卤素，氰基，C 1-6烷基，C 1-6烷氧基，Ar-氧基，C 1-6烷硫基，二（C 1-6烷基）氨基，三卤甲基，三卤甲氧基， 可形成二价基团; R5是被氢或C1-6烷基取代的咪唑基; R6，氢，羟基，卤素，氰基，任选取代的C 1-6烷基，C 1-6烷氧基羰基或Ar; 或式-O-R7，-S-R8，-N-R8R9的基团; 和Ar是任选取代的苯基; 具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 2. 发明授权
      US06444812B1 Intermediate compounds in the preparation of farnnesyl transferase inhibiting 1,8-annelated quinolinone derivatives substituted with N-or C linked imidazoles 有权
    • Intermediate compounds in the preparation of farnnesyl transferase inhibiting 1,8-annelated quinolinone derivatives substituted with N-or C linked imidazoles
    • 中间体化合物制备法尼烯基转移酶抑制被N-或C连接的咪唑取代的1,8-环化喹啉酮衍生物
    • US06444812B1
    • 2002-09-03
    • US09725391
    • 2000-11-29
    • Marc Gaston Venet , Patrick René Angibaud , Yannick Aimé Eddy Ligny , Virginie Sophie Poncelet , Gerard Charles Sanz
    • Marc Gaston Venet , Patrick René Angibaud , Yannick Aimé Eddy Ligny , Virginie Sophie Poncelet , Gerard Charles Sanz
    • C07D26538
    • C07D471/06 , C07D455/04
    • This invention concerns intermediates in the preparation of compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; —A— is a bivalent radical of formula; R1 and R2 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar, Ar—C1-6alkyl, Ar-oxy, Ar—C1-6alkyloxy; or when on adjacent positions R1 and R2 taken together may form a bivalent radical; R3 and R4 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy, Ar-oxy, C1-6alkylthio, di(C1-6alkyl)amino, trihalomethyl, trihalomethoxy, or when on adjacent positions R3 and R4 taken together may form a bivalent radical; R5 is an imidazolyl substituted with hydrogen or C1-6alkyl; R6 hydrogen, hydroxy, halo, cyano, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl or Ar; or a radical of formula —O—R7, —S—R8, —N—R8R9; and Ar is optionally substituted phenyl; and of the preparation, thereof.
    • 本发明涉及制备药学上可接受的酸加成盐及其立体化学异构形式的化合物的中间体，其中虚线表示任选的键; X是氧或硫; -A-是式的二价基团; R 1和R 2各自独立地为氢，羟基，卤素，氰基，C 1-6烷基，三卤代甲基，三卤甲氧基，C 2-6烯基，C 1-6烷氧基，羟基C 1-6烷氧基，C 1-6烷氧基C 1-6烷氧基，C 1-6烷氧基羰基，氨基C 1-6烷氧基， 或二（C 1-6烷基）氨基C 1-6烷氧基，Ar，Ar-C 1-6烷基，Ar-氧基，Ar-C 1-6烷氧基; 或者当在相邻位置R1和R2一起可以形成二价基团时; R 3和R 4各自独立地为氢，卤素，氰基，C 1-6烷基，C 1-6烷氧基，Ar-氧基，C 1-6烷硫基，二（C 1-6烷基）氨基，三卤甲基，三卤甲氧基， 可形成二价基团; R5是被氢或C1-6烷基取代的咪唑基; R6，氢，羟基，卤素，氰基，任选取代的C 1-6烷基，C 1-6烷氧基羰基或Ar; 或式-O-R7，-S-R8，-N-R8R9的基团; 和Ar是任选取代的苯基; 及其制备方法。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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